scholarly journals In Vitro Drug Release, Permeability, and Structural Test of Ciprofloxacin-Loaded Nanofibers

Pharmaceutics ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 556
Author(s):  
Luca Éva Uhljar ◽  
Sheng Yuan Kan ◽  
Norbert Radacsi ◽  
Vasileios Koutsos ◽  
Piroska Szabó-Révész ◽  
...  
Keyword(s):  
Amorphous State ◽  
Physical Mixture ◽  
Water Soluble ◽  
Vinyl Pyrrolidone ◽  
Amorphous Solid Dispersion ◽  
Release Mechanism ◽  
Dissolution Studies ◽  
In Vitro Diffusion ◽  
Poly Vinyl Pyrrolidone

Nanofibers of the poorly water-soluble antibiotic ciprofloxacin (CIP) were fabricated in the form of an amorphous solid dispersion by using poly(vinyl pyrrolidone) as a polymer matrix, by the low-cost electrospinning method. The solubility of the nanofibers as well as their in vitro diffusion were remarkably higher than those of the CIP powder or the physical mixture of the two components. The fiber size and morphology were optimized, and it was found that the addition of the CIP to the electrospinning solution decreased the nanofiber diameter, leading to an increased specific surface area. Structural characterization confirmed the interactions between the drug and the polymer and the amorphous state of CIP inside the nanofibers. Since the solubility of CIP is pH-dependent, the in vitro solubility and dissolution studies were executed at different pH levels. The nanofiber sample with the finest morphology demonstrated a significant increase in solubility both in water and pH 7.4 buffer. Single medium and two-stage biorelevant dissolution studies were performed, and the release mechanism was described by mathematical models. Besides, in vitro diffusion from pH 6.8 to pH 7.4 notably increased when compared with the pure drug and physical mixture. Ciprofloxacin-loaded poly(vinyl pyrrolidone) (PVP) nanofibers can be considered as fast-dissolving formulations with improved physicochemical properties.

scholarly journals Novel Gliclazide Electrosprayed Nano-Solid Dispersions: Physicochemical Characterization and Dissolution Evaluation

2019 ◽  
Vol 9 (2) ◽  
pp. 231-240
Author(s):  
Khosro Adibkia ◽  
Solmaz Ghajar ◽  
Karim Osouli-Bostanabad ◽  
Niloufar Balaei ◽  
Shahram Emami ◽  
...  
Keyword(s):  
Drug Release ◽  
Solid Dispersions ◽  
In Vitro Release ◽  
Physicochemical Characterization ◽  
Amorphous State ◽  
Water Soluble ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Peg 6000

Purpose: In the current study, electrospraying was directed as a novel alternative approach to improve the physicochemical attributes of gliclazide (GLC), as a poorly water-soluble drug, by creating nanocrystalline/amorphous solid dispersions (ESSs). Methods: ESSs were formulated using Eudragit® RS100 and polyethylene glycol (PEG) 6000 as polymeric carriers at various drug: polymer ratios (i.e. 1:5 and 1:10) with different total solution concentrations of 10, 15, and 20% w/v. Morphological, physicochemical, and in-vitro release characteristics of the developed formulations were assessed. Furthermore, GLC dissolution behaviors from ESSs were fitted to various models in order to realize the drug release mechanism. Results: Field emission scanning electron microscopy analyses revealed that the size and morphology of the ESSs were affected by the drug: polymer ratios and solution concentrations. The polymer ratio augmentation led to increase in the particle size while the solution concentration enhancement yielded in a fiber establishment. Differential scanning calorimetry and powder X-ray diffraction investigations demonstrated that the ESSs were present in an amorphous state. Furthermore, the in vitro drug release studies depicted that the samples prepared employing PEG 6000 as carrier enhanced the dissolution rate and the model that appropriately fitted the release behavior of ESSs was Weibull model, where demonstrating a Fickian diffusion as the leading release mechanism. Fourier-transform infrared spectroscopy results showed a probability of complexation or hydrogen bonding, development between GLC and the polymers in the solid state. Conclusion: Hence the electrospraying system avails the both nanosizing and amorphization advantages, therefore, it can be efficiently applied to formulating of ESSs of BCS Class II drugs.

scholarly journals Potential Implantable Nanofibrous Biomaterials Combined with Stem Cells for Subchondral Bone Regeneration

Materials ◽  
2020 ◽  
Vol 13 (14) ◽  
pp. 3087
Author(s):  
Rana Smaida ◽  
Luc Pijnenburg ◽  
Silvia Irusta ◽  
Erico Himawan ◽  
Gracia Mendoza ◽  
...  
Keyword(s):  
Stem Cells ◽  
Bone Regeneration ◽  
Subchondral Bone ◽  
Therapeutic Potential ◽  
Sodium Hyaluronate ◽  
Vinyl Pyrrolidone ◽  
Regenerative Ability ◽  
Poly Vinyl Pyrrolidone

The treatment of osteochondral defects remains a challenge. Four scaffolds were produced using Food and Drug Administration (FDA)-approved polymers to investigate their therapeutic potential for the regeneration of the osteochondral unit. Polycaprolactone (PCL) and poly(vinyl-pyrrolidone) (PVP) scaffolds were made by electrohydrodynamic techniques. Hydroxyapatite (HAp) and/or sodium hyaluronate (HA) can be then loaded to PCL nanofibers and/or PVP particles. The purpose of adding hydroxyapatite and sodium hyaluronate into PCL/PVP scaffolds is to increase the regenerative ability for subchondral bone and joint cartilage, respectively. Human bone marrow-derived mesenchymal stem cells (hBM-MSCs) were seeded on these biomaterials. The biocompatibility of these biomaterials in vitro and in vivo, as well as their potential to support MSC differentiation under specific chondrogenic or osteogenic conditions, were evaluated. We show here that hBM-MSCs could proliferate and differentiate both in vitro and in vivo on these biomaterials. In addition, the PCL-HAp could effectively increase the mineralization and induce the differentiation of MSCs into osteoblasts in an osteogenic condition. These results indicate that PCL-HAp biomaterials combined with MSCs could be a beneficial candidate for subchondral bone regeneration.

Formulation and evaluation of proniosome loaded sertaconazole nitrate for topical application

2021 ◽  
Vol 1 (2) ◽  
pp. 023-037
Author(s):  
Shailaja D ◽  
Latha K ◽  
Manasa D ◽  
Shirisha A ◽  
Padmavathi R ◽  
...  
Keyword(s):  
Ex Vivo ◽  
Release Kinetics ◽  
Skin Irritation ◽  
Water Soluble ◽  
Ionic Surfactants ◽  
Release Mechanism ◽  
Stability Studies ◽  
Zero Order Release ◽  
Poorly Soluble

Proniosomal technology is a novel solution for poorly soluble drugs. Proniosomes are water-soluble carrier particles which are coated with non-ionic surfactants. Proniosomal gels were prepared by coacervation phase separation method using non-ionic surfactants, lipid carriers and cholesterol as a membrane stabilizer. FTIR compatibility studies revealed that the drug and excipients were compatible. All formulations were evaluated for pH, drug content, extrudability, spreadability, viscosity, in-vitro, ex-vivo, skin irritation and stability studies. Among formulations prepared, F80H1 has shown higher % EE (83.02) and least diffusion through dialysis membrane i.e., 17.68%. With ex-vivo studies, F80H1 formulation has shown highest skin deposition and lower flux of sertaconazole nitrate through the rat skin. F80H1 was selected as final optimized formulation. F80H1 exhibited good stability and SEM studies revealed that the vesicles were spherical in shape. The optimized formulation was found to follow zero order release kinetics and korsmeyer-peppas release mechanism. F80H1 found to be non-irritant and stable from skin irritation and stability studies.

scholarly journals PREPARATION AND CHARACTERIZATION OF POLY (VINYL ALCOHOL)–POLY (VINYL PYRROLIDONE) MUCOADHESIVE BUCCAL PATCHES FOR DELIVERY OF LIDOCAINE HCL

2018 ◽  
Vol 10 (1) ◽  
pp. 115 ◽  
Author(s):  
Napaphak Jaipakdee ◽  
Thaned Pongjanyakul ◽  
Ekapol Limpongsa
Keyword(s):  
Vinyl Alcohol ◽  
Vinyl Pyrrolidone ◽  
Poly Vinyl Alcohol ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Casting Technique ◽  
In Vitro Permeation ◽  
Lidocaine Hcl ◽  
Poly Vinyl Pyrrolidone

Objective: The objectives of this study were to prepare and characterize a buccal mucoadhesive patch using poly (vinyl alcohol) (PVA), poly (vinyl pyrrolidone) (PVP) as a mucoadhesive matrix, Eudragit S100 as a backing layer, and lidocaine HCl as a model drug.Methods: Lidocaine HCl buccal patches were prepared using double casting technique. Molecular interactions in the polymer matrices were studied using attenuated total reflectance-fourier transform infrared spectroscopy (ATR-FTIR), differential scanning calorimetry (DSC) and X-ray diffractometry. Mechanical and mucoadhesive properties were measured using texture analyzer. In vitro permeation of lidocaine HCl from the patch was conducted using Franz diffusion cell.Results: Both of the free and lidocaine HCl patches were smooth and transparent, with good flexibility and strength. ATR-FTIR, DSC and X-ray diffractometry studies confirmed the interaction of PVA and PVP. Mechanical properties of matrices containing 60% PVP were significantly lower than those containing 20% PVP (*P<0.05). Mucoadhesive properties had a tendency to decrease with the concentration of PVP in the patch. The patch containing 60% PVP had significantly lower muco-adhesiveness than those containing 20% PVP (*P<0.05). In vitro permeation revealed that the pattern of lidocaine HCl permeation started with an initial fast permeation, followed by a slower permeation rate. The initial permeation fluxes follow the zero-order model of which rate was not affected by the PVP concentrations in the PVA/PVP matrix.Conclusion: Mucoadhesive buccal patches fabricated with PVA/PVP were successfully prepared. Incorporation of PVP in PVA/PVP matrix affected the strength of polymeric matrix and mucoadhesive property of patches.

scholarly journals Fabrication Of Glimepiride Datura Stramonium Leaves Mucilage And Poly Vinyl Pyrrolidone Sustained Release Matrix Tablets: In Vitro Evaluation

1970 ◽  
Vol 8 (1) ◽  
pp. 63-72
Author(s):  
Abdul Ahad Hindustan ◽  
U Anand Babu ◽  
K Nagesh ◽  
D Sai Kiran ◽  
K Bindu Madhavi
Keyword(s):  
Mechanical Properties ◽  
Sustained Release ◽  
Datura Stramonium ◽  
Matrix Tablets ◽  
Vinyl Pyrrolidone ◽  
Stability Studies ◽  
Swelling Properties ◽  
Accelerated Stability ◽  
Poly Vinyl Pyrrolidone

The main purpose of the present work was to develop matrix tablets of Glimepiride with Datura stramonium leaves mucilage and Poly Vinyl Pyrrolidone and to study its functionality as a matrix forming agent for sustained release tablet formulations. Mucilage from Datura stramonium leaves was extracted, isolated, purified and characterized. Physicochemical properties of the dried powdered mucilage of Datura stramonium leaves were studied. Various formulations of Glimepiride Datura stramonium leave mucilage and Poly Vinyl Pyrrolidone were prepared. The formulated tablets were tested for mechanical properties, friability, swelling behavior, in vitro drug release pattern and the dissolution data was treated with mathematical modeling and the optimized formulation was tested for accelerated stability studies. The formulated tablets were found to have good mechanical properties, good swelling properties. The in vitro dissolution data was perfectly fitting to zero order and the release of drug from the formulation followed Higuchi’s release. The accelerated stability studies revealed that the tablets retain their characteristics even after stressed storage conditions. From this study it was concluded that the dried Datura stramonium leaves mucilage and Poly Vinyl Pyrrolidone combination can be used as a matrix forming material for making sustained release matrix tablets. DOI: http://dx.doi.org/10.3126/kuset.v8i1.6044 KUSET 2012; 8(1): 63-72

scholarly journals Amorphous solid dispersions and the confounding effect of nanoparticles in in vitro dissolution and in vivo testing: Niclosamide as a case of study

2020 ◽  
Author(s):  
Miguel O Jara ◽  
Zachary N Warnken ◽  
Robert O Williams
Keyword(s):  
Amorphous Solid ◽  
Fold Increase ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Amorphous Solid Dispersion ◽  
In Vitro Tests ◽  
Manufacturing Method ◽  
Poorly Water Soluble

We developed an amorphous solid dispersion (ASD) of the poorly water soluble molecule niclosamide that achieved more than a 2 fold increase in bioavailability. Notably, this niclosamide ASD formulation increased the apparent drug solubility about 60 fold relative to the crystalline material due to the generation of nanoparticles. Niclosamide is a weakly acidic drug, BCS class II, and a poor glass former with low bioavailability in vivo. Hot melt extrusion is a high throughput manufacturing method commonly used in the development of ASDs for increasing the apparent solubility and bioavailability of poorly water-soluble compounds. We utilized the polymer polyvinylpyrrolidone vinyl acetate (PVPVA) to manufacture niclosamide ASDs by extrusion. Samples were analyzed based on their microscopic and macroscopic behavior and their intermolecular interactions, using DSC, XRD, NMR, FTIR, and DLS. The niclosamide ASD generated nanoparticles with a mean particle size of about 100 nm in FaSSIF media. In a side by side diffusion test, these nanoparticles produced a 4 fold increase in niclosamide diffusion. We successfully manufactured amorphous extrudates of the poor glass former niclosamide that showed remarkable in vitro dissolution and diffusion performance. These in vitro tests were translated to a rat model that also showed an increase in oral bioavailability.

scholarly journals Fabrication of Supercritical Antisolvent (SAS) Process-Assisted Fisetin-Encapsulated Poly (Vinyl Pyrrolidone) (PVP) Nanocomposites for Improved Anticancer Therapy

Nanomaterials ◽  
2020 ◽  
Vol 10 (2) ◽  
pp. 322 ◽  
Author(s):  
Lin-Fei Chen ◽  
Pei-Yao Xu ◽  
Chao-Ping Fu ◽  
Ranjith Kumar Kankala ◽  
Ai-Zheng Chen ◽  
...  
Keyword(s):  
Pharmaceutical Formulations ◽  
Vinyl Pyrrolidone ◽  
Solution Flow Rate ◽  
Therapeutic Effects ◽  
Mass Ratio ◽  
Scanning Calorimetry ◽  
Solution Flow ◽  
Supercritical Antisolvent ◽  
Poly Vinyl Pyrrolidone

Due to its hydrophobicity, fisetin (FIS) often suffers from several limitations in terms of its applicability during the fabrication of pharmaceutical formulations. To overcome this intrinsic limitation of hydrophobicity, we demonstrate here the generation of poly (vinyl pyrrolidone) (PVP)-encapsulated FIS nanoparticles (FIS-PVP NPs) utilizing a supercritical antisolvent (SAS) method to enhance its aqueous solubility and substantial therapeutic effects. In this context, the effects of various processing and formulation parameters, including the solvent/antisolvent ratio, drug/polymer (FIS/PVP) mass ratio, and solution flow rate, on the eventual particle size as well as on distribution were investigated using a 23 factorial experimental design. Notably, the FIS/PVP mass ratio significantly affected the morphological attributes of the resultant particles. Initially, the designed constructs were characterized systematically using various techniques (e.g., chemical functionalities were examined with Fourier-transform infrared (FTIR) spectroscopy, and physical states were examined with X-ray diffraction analysis (XRD) and differential scanning calorimetry (DSC) techniques). In addition, drug release as well as cytotoxicity evaluations in vitro indicated that the nanosized polymer-coated particles showed augmented performance efficiency compared to the free drug, which was attributable to the improvement in the dissolution rate of the FIS-PVP NPs due to their small size, facilitating a higher surface area over the raw form of FIS. Our findings show that the designed SAS process-assisted nanoconstructs with augmented bioavailability, have great potential for applications in pharmaceutics.

Development and Evaluation of Sustained Release Matrix Tablets of Tramadol Hydrochloride

1970 ◽  
Vol 9 (4) ◽  
pp. 3364-3371
Author(s):  
Ganesh Basarkar ◽  
Vijay Suryawanshi ◽  
Dinesh Hire
Keyword(s):  
Calcium Phosphate ◽  
Drug Release ◽  
Sustained Release ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Matrix System ◽  
Tramadol Hydrochloride ◽  
Sustained Release Formulation

The objective of the present study was to control the release of freely water soluble Tramadol hydrochloride over a prolonged period of time by embedding the drug into novel wax matrix system. The matrix granules were prepared by melt granulation technique. The need for the administration two to four times a day when larger dose are required can decrease patient compliance. Sustained release formulation that would maintain plasma levels for 24 hrs for once daily dosing of Tramadol hydrochloride was prepared. The compatibility of the drug and wax examined using Differential Scanning Calorimetry (DSC) and Fourier Transform Infrared Spectrophotometer (FTIR). The effect of wax concentration (5 to 35%) and channeling agents (Avicel PH-101 and Di-calcium phosphate) on the in vitro drug release at 24 hrs. was studied.  Results of DSC confirmed drug-wax compatibility. Increasing the wax concentration resulted in a significant retardation of drug release. The drug release study revealed that the optimized formulation (F6) 30% novel wax sustained drug release for 24hrs. At the same wax concentration, drug release from tablets decreased with Di-calcium phosphate and increased with Avicel PH 101. Kinetic modeling of in vitro dissolution profiles revealed the drug release mechanism ranges from diffusion controlled or Fickian transport to anomalous type or non-Fickian transport. A hydrophobic matrix system is thus useful technique for prolonging the drug release of freely water soluble drugs such as Tramadol hydrochloride

scholarly journals DEVELOPMENT AND EVALUATION OF MONOLITHIC OSMOTIC TABLET OF KETOPROFEN: USING SOLID DISPERSION TECHNIQUE

2016 ◽  
Vol 8 (12) ◽  
pp. 41
Author(s):  
S. Kaushik ◽  
Kamla Pathak
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Amorphous State ◽  
Immediate Release ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
Peg 6000 ◽  
Environmental Media ◽  
Dispersion Technique

<p><strong>Objective: </strong>The aim of the present study was to develop and evaluate the monolithic osmotic tablet (MOT) composed of the solid dispersion of ketoprofen (KETO), a poorly water-soluble drug. Solid dispersion technique is generally used for immediate release, as this maximizes the amount of drug absorbed. Sustained release may be obtained by combining solid dispersion technique with MOT so as to increase the therapy efficacy and patient compliance.</p><p><strong>Methods: </strong>Solid dispersion of KETO was prepared by using solvent melt method with polyethylene glycol (PEG) 6000, a hydrophilic carrier. The ratio of KETO to PEG 6000 were 1:1, 1:3 and 1:5 (%w/w). These solid dispersions were characterized by differential scanning calorimetry (DSC), Thermogravimetric analysis (TGA) and powder X-ray diffraction (PXRD) to ascertain whether there were any physicochemical interactions between drug and carrier.</p><p>The tablet core was prepared by using Polyox N80 (a suspending agent), sodium chloride (an osmotic agent), a solid dispersion consisting of PEG 6000 and KETO followed by a coating of cellulose acetate to make the monolithic osmotic tablet.</p><p><strong>Results: </strong>The results of DSC and PXRD indicated that the drug was in the amorphous state in solid dispersion when PEG 6000 was used as a carrier. The dissolution rate of the solid dispersion was much faster than those for the corresponding physical mixture and pure drug. The optimized MOT formulations were able to deliver KETO at the constant zero order release, above 95% <em>in vitro</em>, independent to environmental media and stirring rate. The release rate of KETO in the MOT is controlled by osmotic pressure, suspending agent and drug solubility in solid dispersion.</p><p><strong>Conclusion: </strong>The monolithic osmotic tablet containing solid dispersion has great potential in the controlled delivery of ketoprofen, a water-insoluble drug.</p><p><strong>Keywords: </strong>Ketoprofen, Monolithic osmotic tablet, Solid dispersion, Water insoluble</p>

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